Neuromuscular relaxants Flashcards
tubocurarine
nondepolarizing, competative, nicotinic receptor antagonist with the longest half life of the curare drugs
this drug is not used clinically
equal elimination from the kidney and liver
pancuronium
nondepolarizing, competative, nicotinic receptor antagonist with a pretty long (over an hour) half life
primarily renal excretion
renal elimination
vecuronium
nondepolarizing, competative, nicotinic receptor antagonist with an hour long half life
primarily renal elimination
mivacurium
nondepolarizing, competative, nicotinic receptor antagonist with a very short half life
complete cholinesterase elimination
rocuronium
nondepolarizing, competative, nicotinic receptor antagonist with an hour long half life
complete liver elimination
clinical uses of non depolarizing, competitive, nicotinic receptor antagonists
surgical procedures (intubation, diaphragm relaxants during mechanical ventilation)
side effects of non depolairzing, competitive, nicotinic receptor antagonists
apnea, non analgesic
succinylcholine
depolarizing nicotinic receptor antagonist that results in prolonged depolarization of the muscle membrane
characteristics of succinylcholine phase 1 block
depolarization of muscle membrane, which results in ~4-8 min of contraction
fluctuating between contraction and relaxation
flaccid paralysis
effect augmented by cholinesterase inhibitors
characteristics of succinylcholine phase 2 block
exposure exceeds 30 min
unknown mechanism results in 0 excitability of the m membrane, despite repolarization
must wait for phase 1 effects to stop (succinylcholine leaves NMJ)
then give cholinesterase inhibitors, which will counteract phase 2 effect
baclofen
GABAb agonist (which does what? where?) administered intrathecally (why?)
benzodiazepines
positive acting GABAa agonist, functions in enhancing the activity of GABAs presynaptic inhibition
tizanidine
alpha2 adrenergic agonist that inhibits both pre and post synaptic transmission of APs
dantrolene
blocks Ca release from the SR by inhibiting RyR used in chronic m spasticity and malignant hyperthermia
malignant hyperthermia
a genetic mutation in the RyR that leads to its overactivation